Channer K S, Virjee J P
J Pharm Pharmacol. 1985 Feb;37(2):126-9. doi: 10.1111/j.2042-7158.1985.tb05021.x.
The oesophageal transit of barium sulphate in small or large, heavy or light capsules or film coated and plain oval tablets was measured during fluoroscopy in five separate studies involving 175 subjects. Transit of large, but not small capsules was significantly faster than plain oval tablets in both erect and supine subjects (P less than 0.05). Heavy large capsules entered the stomach in all subjects within 20 s, whereas in all other studies some subjects retained dosage forms in the oesophagus for over 5 min. The transit of heavy capsules was significantly faster than light capsules in erect subjects (P less than 0.0005). Light capsules tended to have faster transit times than heavy capsules in the supine position. Film coating significantly enhanced oval tablet transit in erect (P less than 0.00003) and supine subjects (P less than 0.05). When large capsules of equal weight but less dense than film coated oval tablets were directly compared, the tablet transit was significantly superior in the erect subjects (P less than 0.0001). In supine subjects the transit of the light capsule was significantly faster (P less than 0.005). It is concluded that different drug formulations can have significant effects on oesophageal transit, and hence on the development of drug induced oesophageal ulceration.
在五项独立研究中,通过荧光透视法对175名受试者服用硫酸钡后在大或小、重或轻的胶囊、薄膜包衣椭圆形片和普通椭圆形片中的食管转运情况进行了测量。在直立和仰卧受试者中,大胶囊(而非小胶囊)的转运速度明显快于普通椭圆形片(P<0.05)。所有受试者服用的大胶囊在胃内20秒内均完成转运,相反,在其他所有测试中,一些受试者服用的剂型在食管内停留超过5分钟。在直立受试者中,重的大胶囊的转运速度明显快于轻的大胶囊(P<0.0005)。在仰卧位时,轻胶囊的转运时间往往比重胶囊快。薄膜包衣显著加快了直立受试者(P<0.00003)和仰卧受试者(P<0.05)中椭圆形片的转运。当直接比较重量相等但密度低于薄膜包衣椭圆形片的大胶囊时,在直立受试者中片剂的转运明显更优(P<0.0001)。在仰卧受试者中,轻胶囊的转运速度明显更快(P<0.005)。得出的结论是,不同的药物制剂对食管转运有显著影响,因此对药物性食管炎的发生也有显著影响。